Methods for making and using pharmaceutical compositions for iontophoresis

Inventors

Kermani, Mahyar Z.

Assignees

Smith and Nephew Orthopaedics AGSmith and Nephew Asia Pacific Pte LtdSmith and Nephew Inc

Publication Number

US-12324792-B2

Publication Date

2025-06-10

Expiration Date

2041-11-05

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Abstract

Methods of making and using pharmaceutical compositions for iontophoresis that include selecting an isotonic pharmaceutical composition that has ions of active and non-active ingredients and reducing/removing the ions of the non-active ingredients from the pharmaceutical composition to produce a revised pharmaceutical composition. The revised pharmaceutical composition is thereafter utilized for iontophoresis in an iontophoresis system. During the step of performing iontophoresis with the revised pharmaceutical composition for a pre-determined dosage, ramp-up period, maximum current, overall time, etc., can be reduced, as compared to performing iontophoresis with the isotonic pharmaceutical composition to provide the pre-determined dosage.

Core Innovation

The invention concerns methods for making and using pharmaceutical compositions tailored for iontophoresis by modifying existing isotonic pharmaceutical compositions. Specifically, the method involves selecting an isotonic pharmaceutical composition that contains ions of active ingredients and competing ions of non-active ingredients, then reducing or removing at least 50% of the competing ions to create a revised pharmaceutical composition. The revised composition is subsequently used for iontophoresis to deliver active ingredients across biological membranes.

The problem addressed is that existing isotonic pharmaceutical compositions used for iontophoresis contain non-active ingredient ions, such as sodium and chloride ions, which act as competing ions. These ions compete with the active ingredient ions during iontophoresis, utilizing some of the current and thus limiting the efficiency of active drug delivery, resulting in longer treatment durations and higher maximum currents needed to achieve a desired drug dosage.

By eliminating or significantly reducing the concentration of competing ions, the revised pharmaceutical composition enables more efficient iontophoretic delivery of active ingredients. This allows for the same or greater drug dosage to be delivered in a shorter application time and at lower maximum currents compared to the use of the original isotonic pharmaceutical composition. Example embodiments demonstrate that profiles involving faster ramp-up periods, reduced steady-state currents, and shorter overall procedure times are achievable with the revised compositions.

Claims Coverage

The patent contains a single independent claim focused on a method for producing and using a modified pharmaceutical composition for iontophoresis by removing competing ions.

Removal of competing ions from isotonic pharmaceutical composition

The inventive feature comprises: 1. Selecting an isotonic pharmaceutical composition that contains charged ions of one or more active ingredients, and competing ions of one or more non-active ingredients. 2. Removing at least 50% molar concentration of the competing ions from the isotonic pharmaceutical composition to create a revised pharmaceutical composition. 3. Utilizing the revised pharmaceutical composition in an iontophoresis system to perform iontophoresis.

The inventive features center on preparing a pharmaceutical composition by reducing or eliminating competing ions, thereby optimizing its use in iontophoresis systems.

Stated Advantages

The method enables reduced maximum current and shorter procedure times for achieving the same or greater drug dosage during iontophoresis, enhancing patient comfort and system efficiency.

Modification of existing isotonic drugs is possible without the need to develop new drugs from scratch, simplifying implementation.

By ramping up more quickly, active ingredients can begin working faster, leading to more rapid onset of therapeutic effect, such as anesthesia.

Reducing or removing competing ions directs more of the applied current to the transport of active ingredients rather than non-active ions, increasing delivery efficiency.

Documented Applications

Iontophoretic drug delivery across biological membranes such as skin and the tympanic membrane, including anesthesia for ear procedures.

Use of modified pharmaceutical compositions (e.g., those containing lidocaine and epinephrine) in iontophoresis systems, including simulated drug delivery in Franz cells.

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